Notch 信號通路廣泛存在于脊椎動物和非脊椎動物,在進化上高度保守,通過相鄰細胞之間的相互作用調節細胞、組織、器官的分化和發育。Notch信號通路由 Notch受體、Notch配體(DSL蛋白)、CSL (CBF-1,Suppressor of hairless,Lag的合稱)DNA結合蛋白、其他的效應物和Notch的調節分子等組成。
DAPT: a γ-secretase inhibitor that blocks Notch signaling. As an inhibitor of Notch, DAPT has been used to study autoimmune and lymphoproliferative diseases, such as ALPS and lupus erythematosus (SLE). As an inhibitor of γ-secretase with IC50 of 0.115 and 0.2 μM for total Aβ and Aβ42 levels, respectively, DAPT may be useful in the study of β-amyloid (Aβ) formation. It is shown to cause a reduction in Aβ40 and Aβ42 levels in human primary neuronal cultures and in brain extract, cerebrospinal fluid and plasma in vivo.
Purity: Greater than 99% as determined by LC/MS analysis. LC/MS and/or NMR data available upon request.
Biological Activity: In a cell-based assay measuring the activation of the Notch pathway reporter gene, this compound gave IC50 of 500 nM.